BRPI0512084A - heterociclos de cinco membros úteis como inibidores de serina protease, composição farmacêutica contendo os mesmos, bem como seu uso - Google Patents

heterociclos de cinco membros úteis como inibidores de serina protease, composição farmacêutica contendo os mesmos, bem como seu uso

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Publication number
BRPI0512084A
BRPI0512084A BRPI0512084-5A BRPI0512084A BRPI0512084A BR PI0512084 A BRPI0512084 A BR PI0512084A BR PI0512084 A BRPI0512084 A BR PI0512084A BR PI0512084 A BRPI0512084 A BR PI0512084A
Authority
BR
Brazil
Prior art keywords
factor
formula
serine protease
compounds
pharmaceutical compositions
Prior art date
Application number
BRPI0512084-5A
Other languages
English (en)
Portuguese (pt)
Inventor
Jon J Hangeland
Mimi L Quan
Joanne M Smallheer
Gregory S Bisacchi
James R Corte
Todd J Friends
Zhong Sun
Karen A Rossi
Cullen L Cavallaro
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35481430&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0512084(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of BRPI0512084A publication Critical patent/BRPI0512084A/pt

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    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P9/06Antiarrhythmics
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    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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Families Citing this family (99)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
US8143425B2 (en) * 2004-10-12 2012-03-27 Bristol-Myers Squibb Company Heterocyclic aromatic compounds useful as growth hormone secretagogues
JP5236293B2 (ja) * 2005-01-13 2013-07-17 ブリストル−マイヤーズ スクイブ カンパニー Xia因子阻害剤としての置換ビアリール化合物
WO2006089005A2 (en) * 2005-02-17 2006-08-24 Bristol-Myers Squibb Company Combination of selective factor viia and/or xia and plasma kallikrein inhibitors
WO2007007588A1 (ja) * 2005-07-08 2007-01-18 Ono Pharmaceutical Co., Ltd. 平面性を有する環状基を母核とする化合物
WO2007008926A1 (en) * 2005-07-11 2007-01-18 Aerie Pharmaceuticals, Inc. Isoquinoline compounds
US20070135499A1 (en) * 2005-07-11 2007-06-14 Aerie Pharmaceuticals, Inc. Hydrazide compounds
EP1966141A1 (en) * 2005-12-14 2008-09-10 Brystol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
US8466295B2 (en) * 2005-12-14 2013-06-18 Bristol-Myers Squibb Company Thiophene derivatives as factor XIa inhibitors
KR20080087817A (ko) * 2005-12-14 2008-10-01 브리스톨-마이어스 스큅 컴퍼니 인자 xia 억제제로서 아릴프로피온아미드,아릴아크릴아미드, 아릴프로핀아미드 또는 아릴메틸우레아유사체
WO2007076161A2 (en) * 2005-12-27 2007-07-05 Myriad Genetics, Inc Compounds with therapeutic activity
PE20080702A1 (es) * 2006-05-16 2008-07-10 Boehringer Ingelheim Int PROLINAMIDAS SUSTITUIDAS COMO INHIBIDORES DEL FACTOR Xa
EP2068878B1 (en) 2006-09-20 2019-04-10 Aerie Pharmaceuticals, Inc. Rho kinase inhibitors
US8410155B2 (en) * 2006-12-15 2013-04-02 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor XIA inhibitors
US8455513B2 (en) * 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
TW200902533A (en) * 2007-05-02 2009-01-16 Boehringer Ingelheim Int Carboxylic acid amides, manufacturing and use thereof as medicaments
CA2687614C (en) * 2007-06-07 2013-04-30 Joyant Pharmaceuticals, Inc. Methods for preparing diazonamides
KR20100037600A (ko) * 2007-06-13 2010-04-09 브리스톨-마이어스 스큅 컴퍼니 응고 인자 억제제로서의 디펩티드 유사체
WO2009064422A2 (en) * 2007-11-13 2009-05-22 Angion Biomedica Corp. Hepatocyte growth factor pathway activators in fibrotic connective tissue diseases
US8455514B2 (en) * 2008-01-17 2013-06-04 Aerie Pharmaceuticals, Inc. 6-and 7-amino isoquinoline compounds and methods for making and using the same
ES2380648T3 (es) * 2008-03-13 2012-05-17 Bristol-Myers Squibb Company Derivados de piridazina como inhibidores del factor XIA
CA2718936A1 (en) * 2008-03-21 2009-09-24 Novartis Ag Novel heterocyclic compounds and uses therof
US8865732B2 (en) 2008-03-21 2014-10-21 Novartis Ag Heterocyclic compounds and uses thereof
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
JP5605844B2 (ja) * 2008-10-17 2014-10-15 塩野義製薬株式会社 血管内皮リパーゼ阻害活性を有する酢酸アミド誘導体
EP2424842B1 (en) 2009-05-01 2015-10-28 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US9206123B2 (en) 2009-12-18 2015-12-08 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
CA2783801A1 (en) * 2009-12-18 2011-06-23 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
PH12012501589A1 (en) 2010-02-11 2012-10-22 Bristol Myers Squibb Co Macrocycles as factor xia inhibitors
US20120046301A1 (en) * 2010-08-20 2012-02-23 Gruenenthal Gmbh Substituted Cyclic Carboxamide and Urea Derivatives as Ligands of the Vanilloid Receptor
CN103221410B (zh) * 2010-09-22 2017-09-15 艾尼纳制药公司 Gpr119受体调节剂和对与其相关的障碍的治疗
US8685966B2 (en) 2011-04-08 2014-04-01 University Of Kansas GRP94 inhibitors
EP2697196A1 (en) 2011-04-13 2014-02-19 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
WO2013006738A1 (en) 2011-07-06 2013-01-10 Gilead Sciences, Inc. Compounds for the treatment of hiv
TW201319068A (zh) 2011-08-05 2013-05-16 必治妥美雅史谷比公司 作為xia因子抑制劑之環狀p1接合劑
TW201311689A (zh) * 2011-08-05 2013-03-16 必治妥美雅史谷比公司 作為因子xia抑制劑之新穎巨環化合物
UY34393A (es) 2011-10-14 2013-04-30 Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor xia
CN103987697B (zh) 2011-10-14 2017-04-26 百时美施贵宝公司 作为因子xia抑制剂的取代的四氢异喹啉化合物
IN2014CN02805A (enExample) 2011-10-14 2015-07-03 Bristol Myers Squibb Co
GB201209138D0 (en) * 2012-05-24 2012-07-04 Ono Pharmaceutical Co Compounds
GB201212081D0 (en) * 2012-07-06 2012-08-22 Kalvista Pharmaceuticals Ltd New polymorph
HRP20161378T1 (hr) 2012-08-03 2016-12-02 Bristol-Myers Squibb Company Dihidropiridon kao faktor xia inhibitora
SI2880026T1 (sl) 2012-08-03 2017-04-26 Bristol-Myers Squibb Company Dihidropiridon p1 kot faktor xia inhibitorjev
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
WO2014059203A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Crystalline forms of a factor xia inhibitor
US9403774B2 (en) 2012-10-12 2016-08-02 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2943487B1 (en) * 2013-01-09 2016-11-16 Gilead Sciences, Inc. 5-membered heteroaryls and their use as antiviral agents
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
PL3811943T3 (pl) 2013-03-15 2023-06-12 Aerie Pharmaceuticals, Inc. Związek do stosowania w leczeniu zaburzeń oczu
US9738655B2 (en) 2013-03-25 2017-08-22 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors
AR097279A1 (es) 2013-08-09 2016-03-02 Actelion Pharmaceuticals Ltd Derivados de benzimidazolil-metil urea como agonistas del receptor de alx
ES2687498T3 (es) 2014-01-31 2018-10-25 Bristol-Myers Squibb Company Macrociclos con grupos P2¿ heterocíclicos como inhibidores del factor XIa
NO2760821T3 (enExample) 2014-01-31 2018-03-10
US9944643B2 (en) 2014-02-11 2018-04-17 Merck Sharp & Dohme Corp. Factor XIa inhibitors
US9676723B2 (en) 2014-02-11 2017-06-13 Merck Sharp & Dohme Corp Factor XIa inhibitors
WO2015130964A1 (en) 2014-02-28 2015-09-03 Gilead Sciences, Inc. Therapeutic compounds
WO2015164308A1 (en) 2014-04-22 2015-10-29 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
US9695166B2 (en) 2014-05-05 2017-07-04 Global Blood Therapeutics, Inc. Pyrazolopyridine pyrazolopyrimidine and related compounds
US9868727B2 (en) 2014-07-28 2018-01-16 Merck Sharp & Dohme Corp. Factor XIa inhibitors
EP3189047B1 (en) 2014-09-04 2018-12-26 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
US10189819B2 (en) 2014-12-10 2019-01-29 Merck Sharp & Dohme, Corp. Factor IXa inhibitors
US9980945B2 (en) 2015-01-13 2018-05-29 Vanderbilt University Benzoisoxazole-substituted compounds as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
WO2016123629A1 (en) 2015-01-30 2016-08-04 Vanderbilt University Indazole and azaindazole substituted compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
CN108026083B (zh) 2015-06-19 2021-08-27 百时美施贵宝公司 作为因子xia抑制剂的二酰胺大环
WO2017019821A1 (en) 2015-07-29 2017-02-02 Bristol-Myers Squibb Company Factor xia new macrocycle bearing a non-aromatic p2' group
WO2017019819A1 (en) 2015-07-29 2017-02-02 Bristol-Myers Squibb Company Factor xia macrocyclic inhibitors bearing alkyl or cycloalkyl p2' moieties
US10344039B2 (en) 2015-10-29 2019-07-09 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor XIa inhibitors, pharmaceutically acceptable compositions and their use
MA43128A (fr) 2015-10-29 2018-09-05 Merck Sharp & Dohme Inhibiteurs du facteur xia
JP6832946B2 (ja) 2015-11-17 2021-02-24 アエリエ ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤およびその中間体の調製方法
US9643927B1 (en) 2015-11-17 2017-05-09 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
PT3347352T (pt) 2016-08-19 2019-09-24 Gilead Sciences Inc Compostos terapêuticos úteis para o tratamento profilático ou terapêutico de uma infeção pelo vírus hiv
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
AU2017317988B2 (en) * 2016-08-31 2020-12-24 Jiangsu Hengrui Medicine Co., Ltd. Oxopicolinamide derivative, preparation method therefor and pharmaceutical use thereof
WO2018045091A1 (en) 2016-08-31 2018-03-08 Aerie Pharmaceuticals, Inc. Ophthalmic compositions
WO2018051306A1 (en) 2016-09-19 2018-03-22 Novartis Ag Therapeutic combinations comprising a raf inhibitor and a erk inhibitor
BR112019020078A2 (pt) 2017-03-31 2020-04-28 Aerie Pharmaceuticals Inc compostos e composições farmacêuticas à base de arilciclopropil-amino-isoquinolinil amida e métodos de uso dos mesmos
EP4272740A1 (en) 2017-05-02 2023-11-08 Novartis AG Combination therapy comprising a raf inhibitor and trametinib
AR112412A1 (es) 2017-08-17 2019-10-23 Gilead Sciences Inc Formas de sal de colina de un inhibidor de la cápside del vih
TW202024061A (zh) 2017-08-17 2020-07-01 美商基利科學股份有限公司 Hiv蛋白質膜抑制劑之固體形式
ES2958828T3 (es) 2018-02-15 2024-02-15 Gilead Sciences Inc Derivados de piridina y su uso para tratar una infección por VIH
AU2019222559B2 (en) 2018-02-16 2022-01-20 Gilead Sciences, Inc. Methods and intermediates for preparing a therapeutic compound useful in the treatment of retroviridae viral infection
US11299462B2 (en) * 2018-02-27 2022-04-12 Jiangsu Hengrui Medicine Co., Ltd. Crystal form of oxopicolinamide derivative and preparation method therefor
SG11202008352YA (en) * 2018-04-10 2020-09-29 Bayer Pharma AG A substituted oxopyridine derivative
CN120078775A (zh) 2018-07-16 2025-06-03 吉利德科学公司 用于治疗hiv的衣壳抑制剂
CA3112391A1 (en) 2018-09-14 2020-03-19 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
JP2022531969A (ja) 2019-05-13 2022-07-12 ノバルティス アーゲー 癌を治療するためのRaf阻害剤としてのN-(3-(2-(2-ヒドロキシエトキシ)-6-モルホリノピリジン-4-イル)-4-メチルフェニル)-2-(トリフルオロメチル)イソニコチンアミドの新規な結晶形態
EP4065116A1 (en) 2019-11-26 2022-10-05 Gilead Sciences, Inc. Capsid inhibitors for the prevention of hiv
CN113683598B (zh) * 2020-05-18 2022-10-14 成都先导药物开发股份有限公司 一种免疫调节剂
JP7520162B2 (ja) 2020-06-25 2024-07-22 ギリアード サイエンシーズ, インコーポレイテッド Hivの治療のためのカプシド阻害剤
TW202342447A (zh) 2021-12-03 2023-11-01 美商基利科學股份有限公司 用於hiv病毒感染之治療性化合物
US12084467B2 (en) 2021-12-03 2024-09-10 Gilead Sciences, Inc. Therapeutic compounds for HIV virus infection
PE20241341A1 (es) 2021-12-03 2024-07-03 Gilead Sciences Inc Compuestos terapeuticos para la infeccion por el virus vih
JP7733916B2 (ja) * 2022-02-28 2025-09-04 学校法人東海大学 Clec-2および/またはgpviの拮抗剤
CN117143081B (zh) * 2022-05-24 2025-08-01 赣南医科大学 一种Sabizabulin的制备方法
CN116891472A (zh) * 2023-07-13 2023-10-17 延边大学 一种含咪唑结构的酰胺类衍生物及其制备方法和应用
WO2025122845A1 (en) * 2023-12-07 2025-06-12 Genep Inc. Imidazole compounds and their use as sodium channel inhibitors

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3255202A (en) * 1963-08-23 1966-06-07 Union Carbide Corp Process for the preparation of 2-(acylamidoalkyl)benzimidazoles
US5618792A (en) 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
JP2000511173A (ja) * 1996-05-27 2000-08-29 藤沢薬品工業株式会社 一酸化窒素産生阻害剤としての新規なインドリルおよびベンゾフラニルカルボキサミド
JP2001505585A (ja) * 1996-12-16 2001-04-24 藤沢薬品工業株式会社 新規アミド化合物およびそれらの一酸化窒素シンターゼ阻害剤としての用途
US6593291B1 (en) 1997-02-06 2003-07-15 Entremed, Inc. Compositions and methods of use of ligands that bind components of the blood coagulation/clotting pathway for the treatment of cancer and angiogenic-based disease
US6740682B2 (en) * 1997-08-29 2004-05-25 Tularik Limited Meta-benzamidine derivatives as serine protease inhibitors
US6852725B1 (en) * 1998-06-12 2005-02-08 Societe De Conseils De Recherches Et D'applications Scientifiques, S. A. S. Imidazolyl derivatives
JP3676677B2 (ja) 1998-06-30 2005-07-27 ファイザー・プロダクツ・インク 炎症性疾患、自己免疫疾患および呼吸疾患の治療において有用なvla−4依存性細胞結合の非ペプチジル阻害薬
EP1126833A4 (en) 1998-10-29 2004-09-08 Trega Biosciences Inc OXADIAZOLE, THIADIAZOLE AND TRIAZOLE DERIVATIVES AND COMBINATORIAL LIBRARIES CONTAINING THESE DERIVATIVES
US6518292B1 (en) 1999-03-12 2003-02-11 Bristol-Myers Squibb Co. Heterocyclic aromatic compounds usefuls as growth hormone secretagogues
TWI283577B (en) 1999-10-11 2007-07-11 Sod Conseils Rech Applic Pharmaceutical composition of imidazole derivatives acting as modulators of sodium channels and the use thereof
US7291641B2 (en) 1999-10-11 2007-11-06 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Derivatives of heterocycles with 5 members, their preparation and their use as medicaments
US6476041B1 (en) 1999-10-29 2002-11-05 Merck & Co., Inc. 1,4 substituted piperidinyl NMDA/NR2B antagonists
EP1226123A1 (en) 1999-11-03 2002-07-31 Du Pont Pharmaceuticals Company Cyano compounds as factor xa inhibitors
EP1244656A1 (en) 1999-12-28 2002-10-02 Pfizer Products Inc. Non-peptidyl inhibitors of vla-4 dependent cell binding useful in treating inflammatory, autoimmune, and respiratory diseases
US20020010140A1 (en) * 2000-01-19 2002-01-24 Striker Gary E. Use of pentosan polysulfate to treat certain conditions of the prostate
CO5271680A1 (es) * 2000-02-21 2003-04-30 Smithkline Beecham Corp Compuestos
ES2218391T3 (es) * 2000-03-06 2004-11-16 Smithkline Beecham Plc Derivados de imidazol como inhibidores de raf-cinasa.
US6414013B1 (en) * 2000-06-19 2002-07-02 Pharmacia & Upjohn S.P.A. Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
KR20030020960A (ko) 2000-08-01 2003-03-10 소시에떼 더 콘세이유 더 레세르세 에 다플리까띠옹 시엔띠피끄, 에스.아.에스. 이미다졸일 유도체
GB0021831D0 (en) 2000-09-06 2000-10-18 Astrazeneca Ab Chemical compounds
KR100673265B1 (ko) * 2000-10-04 2007-01-22 엘지.필립스 엘시디 주식회사 액정표시장치
CN100581544C (zh) 2001-03-05 2010-01-20 美国医疗产品公司 用于勃起机能障碍治疗和逆转的可注射药物组合物
JP2004523565A (ja) 2001-03-05 2004-08-05 トランス テック ファーマ,インコーポレイテッド 治療因子としてのベンゾイミダゾール誘導体
CA2450579A1 (en) 2001-06-20 2003-01-03 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
WO2003035615A2 (en) 2001-10-25 2003-05-01 Merck & Co., Inc. Tyrosine kinase inhibitors
DE10211770A1 (de) 2002-03-14 2003-10-02 Boehringer Ingelheim Pharma Neue substituierte Piperidine, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
AU2003254781A1 (en) 2002-07-31 2004-02-16 Nippon Soda Co., Ltd. Aminosalicylamide derivative, process for producing the same and agri-horticultural pesticide
AU2003265585B2 (en) * 2002-08-26 2008-07-03 Takeda Pharmaceutical Company Limited Calcium receptor modulating compound and use thereof
PE20040804A1 (es) 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
US20040186151A1 (en) 2003-02-12 2004-09-23 Mjalli Adnan M.M. Substituted azole derivatives as therapeutic agents
US7138412B2 (en) 2003-03-11 2006-11-21 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives useful as serine protease inhibitors
BRPI0407926A (pt) 2003-03-27 2006-02-21 Pfizer Prod Inc 4-amino[1,2,4]triazol[4,3-a]quinoxalinas substituìdas
JP2004323516A (ja) * 2003-04-11 2004-11-18 Nippon Soda Co Ltd 3−アシルアミノサリチル酸アミド誘導体、製造法及び農園芸用殺菌剤
US7129264B2 (en) 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
EP1479679A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Triazole-derivatives as factor Xa inhibitors
JP2007507464A (ja) 2003-10-01 2007-03-29 アルタナ ファルマ アクチエンゲゼルシャフト 新規のアミノピリジン誘導体
US7128412B2 (en) * 2003-10-03 2006-10-31 Xerox Corporation Printing processes employing intermediate transfer with molten intermediate transfer materials
AR046787A1 (es) 2003-12-05 2005-12-21 Bristol Myers Squibb Co Agentes antimigrana heterociclicos
US7371743B2 (en) 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
JP5236293B2 (ja) 2005-01-13 2013-07-17 ブリストル−マイヤーズ スクイブ カンパニー Xia因子阻害剤としての置換ビアリール化合物
KR20080087817A (ko) 2005-12-14 2008-10-01 브리스톨-마이어스 스큅 컴퍼니 인자 xia 억제제로서 아릴프로피온아미드,아릴아크릴아미드, 아릴프로핀아미드 또는 아릴메틸우레아유사체

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